Drug Information | Therapeutic Target Database

Drug General Information

Drug ID

D0B9EH

Former ID

DCL000019

Drug Name

Dermolastin

Synonyms

Dermolastin

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Drug Type

Small molecular drug

Indication

Atopic dermatitis [ICD-11: EA80; ICD-10: L20; ICD-9: 691.8, 692.9]

Discontinued in Phase 2

[1]

Company

Arriva Pharma

Structure

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2D MOL

Formula

C27H31NOS2

Canonical SMILES

CCN(CC=CC#CC(C)(C)C)CC1=CC(=CC=C1)OCC2=CC(=CS2)C3=CSC=C3

InChI

1S/C27H31NOS2/c1-5-28(14-8-6-7-13-27(2,3)4)18-22-10-9-11-25(16-22)29-19-26-17-24(21-31-26)23-12-15-30-20-23/h6,8-12,15-17,20-21H,5,14,18-19H2,1-4H3

InChIKey

KIRGLCXNEVICOG-UHFFFAOYSA-N

PubChem Compound ID

188403

PubChem Substance ID

Target and Pathway

Target(s)

Cathepsin G (CTSG)

Target Info

Inhibitor

[2], [3], [4], [5]

Cationic trypsinogen (PRSS1)

Target Info

Inhibitor

[2], [3], [4], [5]

Coagulation factor IIa (F2)

Target Info

Inhibitor

[2], [3], [4], [5]

Neutrophil elastase (NE)

Target Info

Inhibitor

[2], [3], [4], [5]

Tissue kallikrein (KLK2)

Target Info

Inhibitor

[2], [3], [4], [5]

KEGG Pathway

Transcriptional misregulation in cancer

Systemic lupus erythematosus

Neuroactive ligand-receptor interaction

Lysosome

Renin-angiotensin system

Amoebiasis

Endocrine and other factor-regulated calcium reabsorption

Pancreatic secretion

Protein digestion and absorption

Influenza A

Complement and coagulation cascades

Regulation of actin cytoskeleton

NetPath Pathway

IL2 Signaling Pathway

TCR Signaling Pathway

Panther Pathway

Blood coagulation

Pathwhiz Pathway

Vitamin K Metabolism

Coagulation

Pathway Interaction Database

Urokinase-type plasminogen activator (uPA) and uPAR-mediated signaling

C-MYB transcription factor network

Coregulation of Androgen receptor activity

Regulation of Androgen receptor activity

Thrombin/protease-activated receptor (PAR) pathway

Angiopoietin receptor Tie2-mediated signaling

FOXA2 and FOXA3 transcription factor networks

PAR4-mediated thrombin signaling events

Syndecan-4-mediated signaling events

PAR1-mediated thrombin signaling events

Reactome

Collagen degradation

Degradation of the extracellular matrix

Activation of Matrix Metalloproteinases

Metabolism of Angiotensinogen to Angiotensins

Regulation of Insulin-like Growth Factor (IGF) transport and uptake by Insulin-like Growth Factor Binding Proteins (IGFBPs)

Activated PKN1 stimulates transcription of AR (androgen receptor) regulated genes KLK2 and KLK3

Cobalamin (Cbl, vitamin B12) transport and metabolism

Intrinsic Pathway of Fibrin Clot Formation

Common Pathway of Fibrin Clot Formation

Gamma-carboxylation of protein precursors

Transport of gamma-carboxylated protein precursors from the endoplasmic reticulum to the Golgi apparatus

Removal of aminoterminal propeptides from gamma-carboxylated proteins

Cell surface interactions at the vascular wall

Peptide ligand-binding receptors

G alpha (q) signalling events

Thrombin signalling through proteinase activated receptors (PARs)

WikiPathways

Hair Follicle Development: Cytodifferentiation (Part 3 of 3)

Human Complement System

Degradation of collagen

ACE Inhibitor Pathway

Regulation of Insulin-like Growth Factor (IGF) Transport and Uptake by Insulin-like Growth Factor Binding Proteins (IGFBPs)

Prostate Cancer

Activation of Matrix Metalloproteinases

Complement and Coagulation Cascades

Regulation of Actin Cytoskeleton

IL1 and megakaryotyces in obesity

PTM: gamma carboxylation, hypusine formation and arylsulfatase activation

Blood Clotting Cascade

Gastrin-CREB signalling pathway via PKC and MAPK

Thrombin signalling through proteinase activated receptors (PARs)

Platelet Aggregation (Plug Formation)

GPCR ligand binding

GPCR downstream signaling

Formation of Fibrin Clot (Clotting Cascade)

Cell surface interactions at the vascular wall

Folate Metabolism

Vitamin B12 Metabolism

Selenium Micronutrient Network

References

REF 1

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018071)

REF 2

Arriva-ProMetic recombinant alpha 1-antitrypsin (rAAT) moves into the clinic for dermatology applications. ProMetic Life Sciences. 2009.

REF 3

rAAt (inhaled) Arriva/Hyland Immuno. Curr Opin Mol Ther. 2006 Feb;8(1):76-82.

REF 4

Optimization of the bioprocessing conditions for scale-up of transient production of a heterologous protein in plants using a chemically inducible viral amplicon expression system. Biotechnol Prog. 2009 May-Jun;25(3):722-34.

REF 5

Bioreactor strategies for improving production yield and functionality of a recombinant human protein in transgenic tobacco cell cultures. Biotechnol Bioeng. 2009 Feb 1;102(2):508-20.

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